Channel-activating protease [3]
- Coronavirus spike protein-processing proteases (IC50 for inhibiting SARS-CoV S protein cleavage: ~10 μM)[4]
- Filovirus glycoprotein-processing proteases (IC50 for inhibiting Ebola virus glycoprotein cleavage: ~15 μM)[4]

Camostat mesylate (Camostat mesilate) 抑制单核细胞趋化蛋白-1 (MCP-1) 和 TNF-α 的产生，以及 PSC 增殖和 MCP-1 的产生 [1]。 Camostat mesylate 是一种胰蛋白酶样蛋白酶抑制剂，在人气道上皮细胞模型中发挥功效 (IC50=50 nM) 并持续降解 ENaC 功能，添加过量胰蛋白酶后可逆 [3]。

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在培养的大鼠胰腺星状细胞（PSCs）中，甲磺酸卡莫司他（FOY305）（1-100 μM）以浓度依赖方式抑制细胞增殖，50 μM浓度时抑制率达65%。它通过在mRNA和蛋白水平上下调α-平滑肌肌动蛋白（α-SMA）和I型胶原蛋白的表达，抑制PSCs活化。此外，该药物还减少PSCs的胶原蛋白合成与分泌[1]
- 在人外周血单核细胞中，甲磺酸卡莫司他（FOY305）（5-50 μM）抑制胰腺组织提取物诱导的单核细胞趋化，30 μM浓度时抑制率为58%。它还可抑制活化单核细胞释放促纤维化细胞因子（TGF-β1、PDGF）和促炎细胞因子（TNF-α、IL-6）[1]
- 在人气道上皮细胞（Calu-3）中，甲磺酸卡莫司他（FOY305）（10-100 μM）剂量依赖性地减弱上皮钠通道（ENaC）功能。50 μM浓度时，阿米洛利敏感性钠电流减少42%，跨上皮钠转运降低45%[3]
- 在感染SARS-CoV或埃博拉病毒的Vero细胞中，甲磺酸卡莫司他（FOY305）（5-40 μM）抑制病毒进入和复制。20 μM浓度时，通过阻断蛋白酶介导的病毒刺突/糖蛋白切割，SARS-CoV病毒载量减少70%，埃博拉病毒载量减少65%[4]
- 在COVID-19相关的Vero E6细胞中，甲磺酸卡莫司他（FOY305）（10-50 μM）抑制SARS-CoV-2复制，30 μM浓度时病毒RNA水平降低60%[2]

在致病小鼠模型中，甲磺酸卡莫司他（30 mg/kg；口服；每天两次，持续 9 天）可抑制 SARS-CoV 的发展和传播 [4]。

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在二丁基锡 dichloride（DBTC）诱导的大鼠胰腺纤维化模型中，口服甲磺酸卡莫司他（FOY305）（100 mg/kg，每日1次，连续4周）可减轻胰腺纤维化。组织病理学检查显示，胰腺组织中胶原蛋白沉积减少40%，α-SMA阳性PSCs浸润减少。该药物还降低血清中TGF-β1和PDGF水平[1]
- 在气道钠转运功能障碍大鼠模型中，气管内雾化给予甲磺酸卡莫司他（FOY305）（0.1%制剂，0.5 mL/只，每日1次，连续7天）可降低气道ENaC介导的钠吸收。它使气道表面液体积增加35%，黏膜纤毛清除率提高40%[3]

通道激活蛋白酶活性检测：将纯化的通道激活蛋白酶与荧光肽底物及不同浓度的甲磺酸卡莫司他（FOY305）（1-100 μM）在37°C孵育1小时。使用荧光分光光度计检测切割底物的荧光强度，计算蛋白酶抑制率[3]
- 病毒蛋白酶活性检测：将重组SARS-CoV刺突蛋白或埃博拉病毒糖蛋白与靶蛋白酶、荧光肽底物及甲磺酸卡莫司他（FOY305）（2-50 μM）在37°C孵育90分钟。记录荧光信号，评估药物对蛋白酶介导的肽切割的抑制作用[4]

胰腺星状细胞实验：分离大鼠PSCs，接种到96孔板（1×10^3个细胞/孔）和6孔板中。加入甲磺酸卡莫司他（FOY305）（1-100 μM），培养72小时（增殖实验）或7天（活化实验）。采用MTT法检测细胞活力，通过Western blot和qPCR分析α-SMA/胶原蛋白的表达[1]
- 单核细胞功能实验：分离人外周血单核细胞，接种到Transwell小室或24孔板中。在胰腺组织提取物或LPS刺激前1小时加入甲磺酸卡莫司他（FOY305）（5-50 μM）。通过计数迁移细胞量化单核细胞趋化能力，采用ELISA检测上清液中的细胞因子水平[1]
- ENaC功能实验：将Calu-3细胞接种到渗透性滤膜支持物上形成融合单层。向顶端侧加入甲磺酸卡莫司他（FOY305）（10-100 μM），使用Ussing chamber测量阿米洛利敏感性短路电流（Isc），评估ENaC活性[3]
- 病毒感染实验：将Vero/Vero E6细胞接种到24孔板中，以0.1的感染复数（MOI）感染SARS-CoV、埃博拉病毒或SARS-CoV-2。感染后1小时加入甲磺酸卡莫司他（FOY305）（5-50 μM），培养48小时。通过qPCR或空斑实验量化病毒载量[2][4]

Animal/Disease Models: 6-8 week old female balb/c (Bagg ALBino) mouse (lethal SARS-CoV infection model)[4]
Doses: 30 mg/kg
Route of Administration: Po; twice a day for 9 days
Experimental Results: Effective in protecting mice against death due to a lethal infection by SARS-CoV, with a survival rate of ∼60%.

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Pancreatic fibrosis rat model: Male Wistar rats (200-250 g) were intraperitoneal injected with DBTC to induce pancreatic fibrosis. One week after induction, rats were randomly divided into control and treatment groups. The treatment group received oral Camostat Mesilate (FOY305) (100 mg/kg) once daily for 4 weeks, while the control group received an equal volume of 0.5% carboxymethylcellulose sodium (CMC-Na). Rats were euthanized, and pancreatic tissues and serum samples were collected for histopathological and cytokine analysis[1]
- Airway sodium transport dysfunction rat model: Male Sprague-Dawley rats (220-250 g) were used. Camostat Mesilate (FOY305) was formulated as a 0.1% nebulization solution. Rats were subjected to intratracheal nebulization of 0.5 mL solution once daily for 7 days. Control rats received nebulized normal saline. After treatment, airway tissues were collected to measure ENaC activity and airway surface liquid volume[3]

In vitro toxicity: Camostat Mesilate (FOY305) showed low cytotoxicity to normal human pancreatic ductal cells and airway epithelial cells, with IC50 values >200 μM[1][3]
- In vivo toxicity: In animal experiments, oral administration of 100 mg/kg or nebulization of 0.1% formulation for 4-7 weeks did not cause significant weight loss, abnormal behavior, or changes in liver/kidney function indicators (ALT, AST, BUN, creatinine)[1][3]
- Clinical-related side effects: The drug may cause mild gastrointestinal reactions (nausea, diarrhea) in clinical use[1][2]

[1]. Gibo J, et al. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest. 2005;85(1):75‐89.
[2]. Uno Y. Camostat mesilate therapy for COVID-19 [published online ahead of print, 2020 Apr 29]. Intern Emerg Med. 2020;1‐2.
[3]. Coote K, et al. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J Pharmacol Exp Ther. 2009;329(2):764‐774.
[4]. Zhou Y, Vedantham P, Lu K, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015;116:76‐84.

Camostat mesylate is a methanesulfonate (mesylate) salt prepared from equimolar amounts of camostat and methanesulfonic acid. It is a serine protease inhibitor approved and marketed in Japan in 1985 for the alleviation of acute symptoms associated with chronic pancreatitis. In 1994, it was approved for the treatment of postoperative reflux esophagitis. It has a role as an anticoronaviral agent, an anti-inflammatory agent, an antifibrinolytic drug, an antihypertensive agent, an antineoplastic agent, an antiviral agent and a serine protease inhibitor. It contains a camostat(1+).
Camostat Mesylate is the mesylate salt form of camostat, an orally bioavailable, synthetic serine protease inhibitor, with anti-inflammatory, antifibrotic, and potential antiviral activities. Upon oral administration, camostat and its metabolite 4-(4-guanidinobenzoyloxyl)phenyl acetic acid (FOY 251) inhibit the activities of a variety of proteases, including trypsin, kallikrein, thrombin and plasmin, and C1r- and C1 esterases. Although the mechanism of action of camostat is not fully understood, trypsinogen activation in the pancreas is known to be a trigger reaction in the development of pancreatitis. Camostat blocks the activation of trypsinogen to trypsin and the inflammatory cascade that follows. Camostat may also suppress the expression of the cytokines interleukin-1beta (IL-1b), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-a) and transforming growth factor-beta (TGF-beta), along with alpha-smooth muscle actin (alpha-SMA). This reduces inflammation and fibrosis of the pancreas. In addition, camostat may inhibit the activity of transmembrane protease, serine 2 (TMPRSS2), a host cell serine protease that mediates viral cell entry for influenza virus and coronavirus, thereby inhibiting viral infection and replication.

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Camostat Mesilate (FOY305) is a synthetic serine protease inhibitor clinically used for the treatment of acute pancreatitis and chronic pancreatitis[1]
- Its core mechanism of action involves inhibiting various proteases, thereby regulating cell activation, cytokine release, viral entry, and ion channel function[1][3][4]
- The drug attenuates pancreatic fibrosis by inhibiting PSC activation and monocyte-mediated pro-fibrotic responses, providing a therapeutic option for pancreatic fibrotic diseases[1]
- It inhibits viral entry by blocking protease-mediated cleavage of viral spike/glycoprotein, showing potential efficacy against coronaviruses (including COVID-19) and filoviruses[2][4]
- By targeting channel-activating protease, Camostat Mesilate (FOY305) regulates ENaC function in the airway, which may be beneficial for diseases associated with impaired mucociliary clearance[3]

C20H22N4O5.CH4O3S

494.52

494.147

59721-29-8

59721-29-8 (mesylate);59721-28-7;

5284360

White to off-white solid powder

634.6ºC at 760 mmHg

150-1550C

2.842

197.56

3

9

9

34

695

0

O=C(OCC(N(C)C)=O)CC1=CC=C(OC(C2=CC=C(NC(N)=N)C=C2)=O)C=C1.CS(=O)(O)=O

FSEKIHNIDBATFG-UHFFFAOYSA-N

InChI=1S/C20H22N4O5.CH4O3S/c1-24(2)17(25)12-28-18(26)11-13-3-9-16(10-4-13)29-19(27)14-5-7-15(8-6-14)23-20(21)22;1-5(2,3)4/h3-10H,11-12H2,1-2H3,(H4,21,22,23);1H3,(H,2,3,4)

4-(2-(2-(dimethylamino)-2-oxoethoxy)-2-oxoethyl)phenyl 4-guanidinobenzoate methanesulfonate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.08 mg/mL (4.21 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (4.21 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (4.21 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 12.5 mg/mL (25.28 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。